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Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
Compound 7n was found to be a potent inhibitor of 11β-hydroxylase (CYP11B1), which is responsible for cortisol production, and is being evaluated in the clinic for potential treatment of hypercortisol diseases such as Cushing's syndrome. Expand
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.
Allosteric dual BRM and BRG1 inhibitors that downregulate BRM-dependent gene expression and show antiproliferative activity in aBRG1-mutant-lung-tumor xenograft model upon oral administration are described. Expand
New synthetic method for the polymerization of alkylthiophenes
Abstract The polymerization of 2-iodo-3-alkylthiophenes using a Heck-type reaction withPd(OAc)2/NBu4Br as catalytic system is reported leading to expected functionalized oligomers with good yields.
[Pterins of Pieridae (Lepidoptera) and their biosynthesis. 3. Study of xanthine dehydrogenase activity (E.C. in the course of development].
In the adult, XDH activity is found in fat body and ovaries of the females, but it seems that only ovaries synthetize pteridines, according to previous labelling experiments. Expand
Ru-catalyzed alkene-alkyne coupling. Total synthesis of amphidinolide P.
A coordinatively unsaturated ruthenium complex catalyzed the formation of a carbon-carbon bond between two judiciously chosen alkene and alkyne partners in good yield, and in a chemo- andExpand
Dinuclear asymmetric Zn aldol additions: formal asymmetric synthesis of fostriecin.
The first application of the recently reported dinuclear Zn-catalyzed direct aldol addition of alkynyl ketones to aldehydes in a short and efficient formal asymmetric synthesis of fostriecin, a potent cyctotoxic natural product is reported. Expand
Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors.
A novel series of aldosterone synthase inhibitors with single-digit nanomolar cellular potency and excellent physicochemical properties are reported and an illustration of the impact of the age of preclinical models on pharmacokinetic properties is highlighted. Expand
Alkene-alkyne coupling as a linchpin: an efficient and convergent synthesis of amphidinolide P.
  • B. Trost, J. Papillon
  • Chemistry, Medicine
  • Journal of the American Chemical Society
  • 30 September 2004
A remarkably chemo- and regioselective ruthenium-catalyzed alkene-alkyne coupling allows for a convergent synthesis and demonstrates that both enynes and beta-lactones are suitable coupling partners. Expand
Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.
This paper summarizes the discovery, pharmacokinetics, and pharmacodynamic data in preclinical species and human subjects of the selective CYP11B2 inhibitor 8. Expand
The preparation of nonracemic secondary alpha-(carbamoyloxy)alkylzinc and copper reagents. A versatile approach to enantioenriched alcohols.
A short, highly efficient synthesis of an industrially relevant pheromone, japonilure, illustrates the value of Hoppe's sBuLi/(-)-sparteine methodology. Expand